Human carboxylesterase (CES) 1 and CES2 are members of the serine hydrolase superfamily, and both exhibit broad substrate specificity and are involved in xenobiotic and endobiotic metabolism. Although expression of CES1 and CES2 occurs in several organs, their expression in liver and small intestine is predominantly attributed to CES1 and CES2, respectively. We successfully expressed CES1 form ...

The in vitro metabolism of tolperisone, 1-(4-methyl-phenyl)-2-methyl-3-(1-piperidino)-1-propanone-hydrochloride, a centrally acting muscle relaxant, was examined in human liver microsomes (HLM) and recombinant enzymes. Liquid chromatography-mass spectrometry measurements revealed methyl-hydroxylation (metabolite at m/z 261; M1) as the main metabolic route in HLM, however, metabolites of two mas...

Heavy liquid metals (HLM) are attractive coolants for nuclear fission and fusion applications due to their excellent thermal properties. In these reactors, a high coolant flow rate must be processed in compact heat exchangers, as such, it may convenient have the HLM flowing on shell side of helical coil steam generator. Technical knowledge about turbulent transfer cross-flow tube bundles is rat...

We aimed to examine the effect of ICT use, parental support and student hindering on science achievement in Turkey, USA South Korea with using PISA 2018 data. is one biggest international assessment study aiming comparison students’ academic capabilities science, mathematics reading among participant countries. For this purpose, we classified variables related -ICT use out school for leisure, c...

Centrifugal pumps are considered to be less destructive to blood elements (1) when compared to roller pumps. However, their large prime volumes render them unsuitable as arterial pumps in heart lung machine (HLM) circuitry for children. In November of 2014, the circuit at Arnold Palmer Hospital, a Biomedicus BP-50 with kinetic assist venous drainage (KAVD) and 1/4″ tubing was converted to a rol...

In vitro metabolism of methadone was investigated in cytochrome P450 (CYP) supersomes and phenotyped human liver microsomes (HLMs) to reconcile past findings on CYP involvement in stereo-selective metabolism of methadone. Racaemic methadone was used for incubations; (R)- and (S)-methadone turnover and (R)- and (S)-EDDP formation were determined using chiral liquid chromatography-tandem mass spe...

The wrist is increasingly being used as the preferred site for objectively assessing physical activity but the relative accuracy of processing methods for wrist data has not been determined. OBJECTIVE This study evaluates the validity of four processing methods for wrist-worn ActiGraph (AG) data against energy expenditure (EE) measured using a portable metabolic analyzer (OM; Oxycon mobile) a...

A higher throughput method of screening for the inhibition of recombinant CYP2D6 using a microtiter plate (MTP) assay was evaluated using 62 new chemical entities and compared to data from the dextromethorphan O-demethylase assay in human liver microsomes (HLM). The IC50 values for the two assays closely matched for 53 compounds (85%). Six of the variant nine compounds had higher IC50 values wi...

Time-dependent inhibition (TDI) of the cytochrome P450 (P450) family of enzymes is usually studied in human liver microsomes (HLM) by investigating whether the inhibitory potency is increased with increased incubation times. The presented work was initiated after a discrepancy was observed for the TDI of an important P450 enzyme, CYP3A4, during early studies of the investigational drug compound...